MY154976A - N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives - Google Patents

N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives

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Publication number
MY154976A
MY154976A MYPI20013310A MYPI20013310A MY154976A MY 154976 A MY154976 A MY 154976A MY PI20013310 A MYPI20013310 A MY PI20013310A MY PI20013310 A MYPI20013310 A MY PI20013310A MY 154976 A MY154976 A MY 154976A
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MY
Malaysia
Prior art keywords
lower alkyl
hydrogen
phenyl
halogen
oxides
Prior art date
Application number
MYPI20013310A
Inventor
Torsten Hoffmann
Sonia Maria Poli
Patrick Schnider
Andrew Sleight
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MY154976A publication Critical patent/MY154976A/en

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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    • C07ORGANIC CHEMISTRY
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pain & Pain Management (AREA)
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  • Addiction (AREA)
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  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

THE INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN R IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY, HALOGEN OR TRIFLUOROMETHYL; R1 IS HYDROGEN OR HALOGEN; OR R AND R1 MAY BE TOGETHER WITH THE RING CARBON ATOMS TO WHICH THEY ARE ATTACHED -CH=CH-CH=CH-; R2 AND R2' ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN, HALOGEN, TRIFLUOROMETHYL, LOWER ALKOXY OR CYANO; OR R2 AND R2' MAY BE TOGETHER -CH=CH-CH=CH-, OPTIONALLY SUBSTITUED BY ONE OR TWO SUBSTITUENTS SELECTED FROM LOWER ALKYL OR LOWER ALKOXY; R3, R3' ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN, LOWER ALKYL OR CYCLOALKYL; R4, R4' ARE INDENPENDENTLY FROM EACH OTHER -(CH2)mOR6 OR LOWER ALKYL; OR R4 AND R4' FORM TOGETHER WITH THE N-ATOM TO WHICH THEY ARE ATTACHED A CYCLIC TERTIARY AMINE OF THE GROUP R5 IS HYDROGEN, HYDROXY, LOWER ALKYL, -LOWER ALKOXY, -(CH2)mOH, -COOR3, -CON(R3)2, -N(R3)CO-LOWER ALKYL OR -C(O)R3; R6 IS HYDROGEN, LOWER ALKYL OR PHENYL; X IS -C(O)N(R6)-, -N(R6)C(O)-, -(CH2)mO- OR -O(CH2)m-; N IS 0, 1, 2, 3 OR 4; AND m IS 1, 2 OR 3; AND TO PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. IT HAS BEEN FOUND THAT THESE COMPOUNDS MAY USED AS PRODRUGS FOR THE TREATMENT OR PREVENTION OF ILLNESSES, RELATED TO THE NK1 RECEPTOR.
MYPI20013310A 2000-07-14 2001-07-12 N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives MY154976A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00115287 2000-07-14

Publications (1)

Publication Number Publication Date
MY154976A true MY154976A (en) 2015-08-28

Family

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Family Applications (1)

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MYPI20013310A MY154976A (en) 2000-07-14 2001-07-12 N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives

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US (4) US6593472B2 (en)
EP (1) EP1303490B1 (en)
JP (1) JP3950044B2 (en)
KR (1) KR100501608B1 (en)
CN (1) CN1178917C (en)
AR (1) AR029717A1 (en)
AT (1) ATE400556T1 (en)
AU (1) AU7061901A (en)
BR (1) BRPI0112475B8 (en)
CA (1) CA2415890C (en)
CY (1) CY1108557T1 (en)
CZ (1) CZ303639B6 (en)
DE (1) DE60134749D1 (en)
DK (1) DK1303490T3 (en)
EC (1) ECSP034431A (en)
EG (1) EG24968A (en)
ES (1) ES2309075T3 (en)
GT (1) GT200100137A (en)
HR (1) HRP20030003B1 (en)
HU (1) HU230316B1 (en)
IL (2) IL153834A0 (en)
JO (1) JO2372B1 (en)
MA (1) MA26929A1 (en)
ME (1) ME01311B (en)
MX (1) MXPA03000366A (en)
MY (1) MY154976A (en)
NO (1) NO324700B1 (en)
NZ (1) NZ523273A (en)
PA (1) PA8522001A1 (en)
PE (1) PE20020272A1 (en)
PL (1) PL205207B1 (en)
PT (1) PT1303490E (en)
RS (1) RS50932B (en)
RU (1) RU2266284C2 (en)
SI (1) SI1303490T1 (en)
UY (1) UY26839A1 (en)
WO (1) WO2002006236A1 (en)
ZA (1) ZA200210207B (en)

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HK1058198A1 (en) 2004-05-07
CN1441782A (en) 2003-09-10
US6593472B2 (en) 2003-07-15
EP1303490B1 (en) 2008-07-09
ATE400556T1 (en) 2008-07-15
US6806370B2 (en) 2004-10-19
PL205207B1 (en) 2010-03-31
MA26929A1 (en) 2004-12-20
ES2309075T3 (en) 2008-12-16
UY26839A1 (en) 2002-01-31
PA8522001A1 (en) 2002-04-25
ZA200210207B (en) 2004-03-17
JP3950044B2 (en) 2007-07-25
CA2415890A1 (en) 2002-01-24
HRP20030003B1 (en) 2011-01-31
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